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补骨脂中分离出的补骨脂素对人肝微粒体CYP1A的选择性抑制作用。

Selective Inhibition of Bakuchicin Isolated from Psoralea corylifolia on CYP1A in Human Liver Microsomes.

作者信息

Kim Sun Joo, Oh Heung Chan, Kim Youn-Chul, Jeong Gil-Saeng, Lee Sangkyu

机构信息

BK21 Plus KNU Multi-Omics based Creative Drug Research Team, College of Pharmacy and Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu 41566, Republic of Korea.

College of Pharmacy, Wonkwang University, Iksan 54538, Republic of Korea.

出版信息

Evid Based Complement Alternat Med. 2016;2016:5198743. doi: 10.1155/2016/5198743. Epub 2016 Feb 9.

DOI:10.1155/2016/5198743
PMID:26977174
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4763008/
Abstract

Bakuchicin is a furanocoumarin isolated from Psoralea corylifolia and shows several biological activities. Although there have been studies on the biological effects of bakuchicin, its modulation potency of CYP activities has not been previously investigated. Here, we investigated the inhibitory effects of bakuchicin on the activities of CYP isoforms by using a cocktail of probe substrates in pooled human liver microsomes (HLMs) and human recombinant cDNA-expressed CYP. Bakuchicin strongly inhibited CYP1A-mediated phenacetin O-deethylation with an IC50 value of 0.43 μM in HLMs. It was confirmed by human recombinant cDNA-expressed CYP1A1 and CYP1A2 with a K i value of 0.11 μM and 0.32 μM, respectively. A Lineweaver-Burk plot indicated that the inhibition mechanism of bakuchicin was competitive inhibition. Overall, this is the first study to investigate the potential CYP1A1 and CYP1A2 inhibition associated with bakuchicin and to report its competitive inhibitory effects on HLMs.

摘要

补骨脂素是从补骨脂中分离出的一种呋喃香豆素，具有多种生物活性。虽然已有关于补骨脂素生物学效应的研究，但其对细胞色素P450（CYP）活性的调节作用尚未见报道。在此，我们通过使用混合人肝微粒体（HLMs）中的探针底物混合物以及人重组cDNA表达的CYP，研究了补骨脂素对CYP同工酶活性的抑制作用。补骨脂素在HLMs中强烈抑制CYP1A介导的非那西丁O - 脱乙基作用，IC50值为0.43μM。通过人重组cDNA表达的CYP1A1和CYP1A2证实，其Ki值分别为0.11μM和0.32μM。Lineweaver - Burk图表明补骨脂素的抑制机制为竞争性抑制。总体而言，这是首次研究补骨脂素对CYP1A1和CYP1A2的潜在抑制作用，并报道其对HLMs的竞争性抑制作用的研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba49/4763008/687fbedbd067/ECAM2016-5198743.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba49/4763008/c9bbec98ec5b/ECAM2016-5198743.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba49/4763008/38a3aeea869f/ECAM2016-5198743.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba49/4763008/fd71bdd5a77a/ECAM2016-5198743.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba49/4763008/d8cb95ee40a5/ECAM2016-5198743.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba49/4763008/687fbedbd067/ECAM2016-5198743.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba49/4763008/c9bbec98ec5b/ECAM2016-5198743.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba49/4763008/38a3aeea869f/ECAM2016-5198743.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba49/4763008/fd71bdd5a77a/ECAM2016-5198743.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba49/4763008/d8cb95ee40a5/ECAM2016-5198743.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba49/4763008/687fbedbd067/ECAM2016-5198743.005.jpg

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